Benzamide therapeutics for the treatment of inflammatory bowel disease

Abstract

Benzamides are disclosed to be useful for treating and preventing inflammatory bowel disease.

What is claimed is:  
     
       1. A method of treatment comprising: 
       a. identifying a patient suffering from or susceptible to an inflammatory bowel condition; and  
       b. administering to said patient in need thereof an effective inflammatory bowel condition-treating amount of a pharmaceutical composition comprising a benzamide compound of Formula I                    
        wherein R′ is a saturated alkyl of from 3 to 5 carbon atoms; each R is independently acetamido, nitro or amino; and n is 1 or 2 as active agent.  
     
     
       2. The method of claim  1  wherein said composition is administered orally. 
     
     
       3. The method of claim  1  wherein said composition is administered parenterally. 
     
     
       4. The method of claim  1  wherein said composition is administered rectally. 
     
     
       5. The method of claim  1  wherein said inflammatory bowel condition is ulcerative colitis. 
     
     
       6. The method of claim  1  wherein said inflammatory bowel condition is Crohn's disease. 
     
     
       7. The method of claim  1  wherein said benzamide is selected from the group consisting of: 
       N-tert-butyl-4-acetamidobenzamide (Compound A);  
       N-iso-propyl-4-acetamidobenzamide (Compound B);  
       N-tert-amyl-4-acetamidobenzamide (Compound C);  
       N-methylcyclopropyl-4-acetamidobenzamide (Compound E);  
       N-iso-propyl-4-nitrobenzamide (Compound F);  
       N-tert-butyl-3-nitrobenzamide (Compound G);  
       N-tert-butyl-2-nitrobenzamide (Compound H);  
       N-n-butyl-4-nitrobenzamide (Compound J);  
       N-n-propyl-4-nitrobenzamide (Compound K);  
       N-tert-butyl-3,5-dinitrobenzamide (Compound L);  
       N-1-methylpropyl-4-nitrobenzamide (Compound M);  
       N-tert-butyl-4-aminobenzamide (Compound N);  
       N-tert-butyl-3-aminobenzamide (Compound P); and  
       N-tert-butyl 4-nitrobenzamide (Compound Q).  
     
     
       8. The method of claim  7  wherein said benzamide is N-tert-butyl-4-acetamidobenzamide (Compound A). 
     
     
       9. A method of treatment comprising: 
       a. identifying a patient suffering from an inflammatory bowel condition; and  
       b. administering to said patient in need thereof an effective inflammatory bowel condition-treating regimen of a pharmaceutical composition comprising a benzamide compound of Formula I                    
        wherein R′ is a saturated alkyl of from 3 to 5 carbon atoms; each R is independently acetamido, nitro or amino; and n is 1 or 2 as active agent.  
     
     
       10. The method of claim  9  wherein said regimen comprises one oral dose per day in an amount of from 0.1 to about 150 mg/kg of patient weight. 
     
     
       11. The method of claim  9  wherein said regimen comprises two or three oral doses per day each in an amount of from 0.1 to about 150 mg/kg of patient weight. 
     
     
       12. The method of claim  9  wherein said regimen comprises one intravenous dose per day in an amount of from about 0.01 mg/kg/hour to about 100 mg/kg/hour of patient weight for at least about 1 hour. 
     
     
       13. The method of claim  9  wherein said regimen comprises two or three intravenous doses per day each in an amount of from about 0.01 mg/kg/hour to about 100 mg/kg/hour of patient weight for at least about 1 hour. 
     
     
       14. The method of claim  9  wherein said regimen comprises one rectal dose per day in an amount of from 1 to about 150 mg/kg of patient weight. 
     
     
       15. The method of claim  9  wherein said regimen comprises two or three rectal doses per day each in an amount of from 1 to about 150 mg/kg of patient weight. 
     
     
       16. A method of prophylaxis comprising: 
       a. identifying a patient susceptible to an inflammatory bowel condition; and  
       b. administering to said patient in need thereof an effective inflammatory bowel condition-treating regimen of a pharmaceutical composition comprising a benzamide compound of Formula I                    
        wherein R′ is a saturated alkyl of from 3 to 5 carbon atoms; each R is independently acetamido, nitro or amino; and n is 1 or 2 as active agent.  
     
     
       17. The method of claim  16  wherein said regimen comprises one oral dose per day in an amount of from 0.1 to about 150 mg/kg of patient weight. 
     
     
       18. The method of claim  16  wherein said regimen comprises two or three oral doses per day each in an amount of from 0.1 to about 150 mg/kg of patient weight. 
     
     
       19. The method of claim  16  wherein said regimen comprises one intravenous dose per day in an amount of from about 0.01 mg/kg/hour to about 100 mg/kg/hour of patient weight for at least about 1 hour. 
     
     
       20. The method of claim  16  wherein said regimen comprises two or three intravenous doses per day each in an amount of from about 0.01 mg/kg/hour to about 100 mg/kg/hour of patient weight for at least about 1 hour. 
     
     
       21. The method of claim  16  wherein said regimen comprises one rectal dose per day in an amount of from 1 to about 150 mg/kg of patient weight. 
     
     
       22. The method of claim  16  wherein said regimen comprises two or three rectal doses per day each in an amount of from 1 to about 150 mg/kg of patient weight.